TY  - JOUR
AU  - Juranić, Ivan
AU  - Tošić, Ana V.
AU  - Kolundžija, Branka
AU  - Drakulić, Branko
PY  - 2014
UR  - https://cer.ihtm.bg.ac.rs/handle/123456789/2670
AB  - Antiproliferative activity of twenty one Michael adducts of aroylacrylic acids and cyclic amines (  N -Me-piperazine, imidazole, 2-Me-imidazole, and indole) was tested toward five human tumor cell lines (HeLa, LS174, K562, FemX, MDA-MB-361) in vitro. Compounds exerted antiproliferative activity in the high to the single-digit micromolar concentrations, causing increase of the cell population fraction in S phase and apoptosis.   N -Me-piperazine and imidazole derivatives of aroylacrylic acids substituted with bulky alkyl substituents (2,4-di-  i -Pr-Ph-, 2,4,6-tri-Et-Ph-, or   β -tetrahydronaphthyl-) showed the best potency, while indole adducts were proved as the inferior antiproliferative agents. Few compounds showed significant selectivity, tumor versus healthy cells, with selectivity index   ∼60  for the most selective congener. An unbiased in silico distinction between more and less potent compounds was obtained from 3D QSAR models derived by alignment-independent GRIND-2 descriptors.
PB  - Springer
T2  - Molecular Diversity
T1  - Antiproliferative activity of the Michael adducts of aroylacrylic acids and cyclic amines
VL  - 18
IS  - 3
SP  - 577
EP  - 592
DO  - 10.1007/s11030-014-9528-4
ER  - 

@article{
author = "Juranić, Ivan and Tošić, Ana V. and Kolundžija, Branka and Drakulić, Branko",
year = "2014",
abstract = "Antiproliferative activity of twenty one Michael adducts of aroylacrylic acids and cyclic amines (  N -Me-piperazine, imidazole, 2-Me-imidazole, and indole) was tested toward five human tumor cell lines (HeLa, LS174, K562, FemX, MDA-MB-361) in vitro. Compounds exerted antiproliferative activity in the high to the single-digit micromolar concentrations, causing increase of the cell population fraction in S phase and apoptosis.   N -Me-piperazine and imidazole derivatives of aroylacrylic acids substituted with bulky alkyl substituents (2,4-di-  i -Pr-Ph-, 2,4,6-tri-Et-Ph-, or   β -tetrahydronaphthyl-) showed the best potency, while indole adducts were proved as the inferior antiproliferative agents. Few compounds showed significant selectivity, tumor versus healthy cells, with selectivity index   ∼60  for the most selective congener. An unbiased in silico distinction between more and less potent compounds was obtained from 3D QSAR models derived by alignment-independent GRIND-2 descriptors.",
publisher = "Springer",
journal = "Molecular Diversity",
title = "Antiproliferative activity of the Michael adducts of aroylacrylic acids and cyclic amines",
volume = "18",
number = "3",
pages = "577-592",
doi = "10.1007/s11030-014-9528-4"
}

Juranić, I., Tošić, A. V., Kolundžija, B.,& Drakulić, B.. (2014). Antiproliferative activity of the Michael adducts of aroylacrylic acids and cyclic amines. in Molecular Diversity
Springer., 18(3), 577-592.
https://doi.org/10.1007/s11030-014-9528-4

Juranić I, Tošić AV, Kolundžija B, Drakulić B. Antiproliferative activity of the Michael adducts of aroylacrylic acids and cyclic amines. in Molecular Diversity. 2014;18(3):577-592.
doi:10.1007/s11030-014-9528-4 .

Juranić, Ivan, Tošić, Ana V., Kolundžija, Branka, Drakulić, Branko, "Antiproliferative activity of the Michael adducts of aroylacrylic acids and cyclic amines" in Molecular Diversity, 18, no. 3 (2014):577-592,
https://doi.org/10.1007/s11030-014-9528-4 . .